The invention relates to a method for producing derivatives of O--glucosylated flavonoid, comprising at least one step of incubating a glucansucrase with a flavonoid and at least one sucrose, the flavonoid being a flavonoid which is monohydroxylated or hydroxylated in a non-vicinal manner on the B cycle. The invention also relates to novel O--glucosylated flavonoid derivatives, and to the use thereof. ##STR00001##

The present invention provides a T-type calcium channel inhibitor which is a compound represented by formula (1), a pharmaceutically acceptable salt of this compound or a solvate of this compound. The present invention also provides: this T-type calcium channel inhibitor; a pharmaceutical product containing this T-type calcium channel inhibitor; and a therapeutic agent or prophylactic agent for diseases, the effective action of which is a T-type calcium channel inhibitory action. (In formula (1), each of R.sup.1 and R.sup.2 independently represents H, OH or OR.sup.11 wherein R.sup.11 represents a C.sub.1-3 alkyl group; each of R.sup.3 and R.sup.4 independently represents H, OH or OR.sup.12, wherein R.sup.12 represents a C.sub.1-3 alkyl group; and each of R.sup.5 and R.sup.6 independently represents H, a halogen atom, a C.sub.1-10 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a phenyl group (which may be substituted by a C.sub.1-6 alkoxy group or a halogen atom), a C.sub.1-3 alkyl-phenyl group (which may be substituted by a C.sub.1-6 alkyloxy group or a halogen atom) or a C.sub.10-50 prenyl group.) ##STR00001##

The present invention provides a T-type calcium channel inhibitor which is a compound represented by formula (1), a pharmaceutically acceptable salt of this compound or a solvate of this compound. The present invention also provides: this T-type calcium channel inhibitor; a pharmaceutical product containing this T-type calcium channel inhibitor; and a therapeutic agent or prophylactic agent for diseases, the effective action of which is a T-type calcium channel inhibitory action. (In formula (1), each of R.sup.1 and R.sup.2 independently represents H, OH or OR.sup.11 wherein R.sup.11 represents a C.sub.1-3 alkyl group; each of R.sup.3 and R.sup.4 independently represents H, OH or OR.sup.12, wherein R.sup.12 represents a C.sub.1-3 alkyl group; and each of R.sup.5 and R.sup.6 independently represents H, a halogen atom, a C.sub.1-10 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a phenyl group (which may be substituted by a C.sub.1-6 alkoxy group or a halogen atom), a C.sub.1-3 alkyl-phenyl group (which may be substituted by a C.sub.1-6 alkyloxy group or a halogen atom) or a C.sub.10-50 prenyl group.) ##STR00001##

The present disclosure provides a semi-synthetic method of dihydroquercetin, belonging to the field of synthesis of organic drugs. The semi-synthetic method includes the following steps: adding quercetin dihydrate to solvent water adjusted to be alkaline with an alkalizing reagent, heating and stirring to dissolve the mixture, and then adding thiourea dioxide under the protection of an inert gas to perform a reduction reaction, to obtain an endpoint reduction reaction solution; diluting the endpoint reduction reaction solution with water and cooling the resultant, and then acidizing, aging, and filtering the resultant to obtain a filtrate and a filter cake; extracting, washing, drying, concentrating, and repeatedly crystallizing the filtrate to obtain dihydroquercetin; and recycling the filter cake after being washed.

The present disclosure provides a semi-synthetic method of dihydroquercetin, belonging to the field of synthesis of organic drugs. The semi-synthetic method includes the following steps: adding quercetin dihydrate to solvent water adjusted to be alkaline with an alkalizing reagent, heating and stirring to dissolve the mixture, and then adding thiourea dioxide under the protection of an inert gas to perform a reduction reaction, to obtain an endpoint reduction reaction solution; diluting the endpoint reduction reaction solution with water and cooling the resultant, and then acidizing, aging, and filtering the resultant to obtain a filtrate and a filter cake; extracting, washing, drying, concentrating, and repeatedly crystallizing the filtrate to obtain dihydroquercetin; and recycling the filter cake after being washed.

The invention discloses novel endocrine treatment phytochemicals which affect androgenic status. The method for treatment of 5-alpha-reductase responsive diseases using four novel 5-alpha-reductase inhibitor compounds; leucoanthocyanidin, glabrene, glabridin, and alpha-terpineol is disclosed. Glabridin does not interfere with normal testosterone to androgen receptor binding.

The invention discloses novel endocrine treatment phytochemicals which affect androgenic status. The method for treatment of 5-alpha-reductase responsive diseases using four novel 5-alpha-reductase inhibitor compounds; leucoanthocyanidin, glabrene, glabridin, and alpha-terpineol is disclosed. Glabridin does not interfere with normal testosterone to androgen receptor binding.

An embodiment of the invention provides a cannabis-based flavonoid pharmaceutical composition including any one or more selected, from among the group of Apigenin, Cannflavin. A. Cannflavin B, Cannflavin C, Chrysoeriol, Cosmosiin, Flavocannabiside, Kaempferol, Luteolin, Myricetin, Orientin, Isoorientin (Homoorientin), Quercetin (+)-Taxifolin, Vitexin, and Isovitexin, or their synthases, for the prevention and treatment of certain cancers that can be treated by therapeutically targeting oncogenic factors including kinases, sirtuins, bromodomains, matrix metalloproteinases and BCL-2. Some of the cancers that can be treated by use of cannabis flavonoids based on the inhibition of these therapeutic targets include brain, breast, colon, renal, liver, lung, pancreatic, prostate, leukemia, melanoma as well as any other cancers that overexpress the oncogenic factors inhibited by the cannabis flavonoids identified herein.

An embodiment of the invention provides a cannabis-based flavonoid pharmaceutical composition including any one or more selected, from among the group of Apigenin, Cannflavin. A. Cannflavin B, Cannflavin C, Chrysoeriol, Cosmosiin, Flavocannabiside, Kaempferol, Luteolin, Myricetin, Orientin, Isoorientin (Homoorientin), Quercetin (+)-Taxifolin, Vitexin, and Isovitexin, or their synthases, for the prevention and treatment of certain cancers that can be treated by therapeutically targeting oncogenic factors including kinases, sirtuins, bromodomains, matrix metalloproteinases and BCL-2. Some of the cancers that can be treated by use of cannabis flavonoids based on the inhibition of these therapeutic targets include brain, breast, colon, renal, liver, lung, pancreatic, prostate, leukemia, melanoma as well as any other cancers that overexpress the oncogenic factors inhibited by the cannabis flavonoids identified herein.

The invention relates to flavanone derivatives, and preparation method and use thereof, particularly relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, a preparation method thereof, and use thereof for preventing or treating a mental disorder or a nervous system disease. The compound of the invention exerts significant activity of inhibiting microglial activation and neuroinflammation, can antagonize dopamine D2 receptor, improve the ethological change in multiple animal models for mental disorders, effectively inhibit neuroinflammation and demyelination, and can be used to prevent or treat a mental disorder and a nervous system disease. ##STR00001##